N-[6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-yl]-1H-indol-6-amine | 1228795-25-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 英文名称: N-[6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-yl]-1H-indol-6-amine
• 英文别名: 6-(1H-indazol-6-yl)-N-(1H-indol-6-yl)imidazo[1,2-a]pyrazin-8-amine
• CAS: 1228795-25-2
• 化学式: C₂₁H₁₅N₇
• 分子量: 365.397
• InChiKey: REGRKEPTFXYWPD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  86.7
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• PYRROLO- AND THIAZOLO-PYRIDINE COMPOUNDS, AND METHODS OF USE THEREOF
  申请人：DENG Shaojiang

  公开号：US20080004309A1

  公开（公告）日：2008-01-03

  The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF).

  这项发明涉及一种能够调节缺氧诱导因子（HIF）稳定性和/或活性的新化合物。
• IMIDAZOPYRAZINE SYK INHIBITORS
  申请人：Mitchell Scott A.

  公开号：US20100152159A1

  公开（公告）日：2010-06-17

  Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

  本文提供了某些咪唑吡嗪化合物及其药物组合物。提供了治疗对Syk活性抑制产生响应的某些疾病和疾病的患者的方法，包括向这些患者施用至少一种有效减少疾病或疾病症状的化学实体的数量。还提供了一种确定样本中Syk激酶存在或不存在的方法。
• IMIDAZOPYRIZINE SYK INHIBITORS
  申请人：Gilead Connecticut, Inc.

  公开号：US20130310363A1

  公开（公告）日：2013-11-21

  Certain imidazopyrazines of Formula (I): or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

  本文提供了公式（I）中的某些咪唑吡嗪化合物或其药学上可接受的盐以及其制药组合物。本文还提供了治疗对Syk活性抑制有反应的某些疾病和障碍的患者的方法，包括向这些患者施用至少一种有效减轻疾病或障碍症状的化学实体的数量。本文还提供了在样品中确定Syk激酶存在或不存在的方法。
• THIAZOLO-PYRIDINE COMPOUNDS AS HIF MODULATORS
  申请人：Fibrogen, Inc.

  公开号：EP3124489A1

  公开（公告）日：2017-02-01

  The present invention relates to novel compounds of formula I wherein: q is 0 or 1; • A is -S- and B is =N-; or • A is =N- and B is -S-; one of -A≃C(R6)- or -B≃C(R6)- is a double bond and the other is a single bond; R1 is selected from the group consisting of hydroxyl, alkoxy, substituted alkoxy, acyloxy, cycloalkoxy, substituted cycloalkoxy, aryloxy, substituted aryloxy, heteroaryloxy, substituted heteroaryloxy, heterocyclyloxy, substituted heterocyclyloxy, mercapto, thioether, sustituted alkylthio, arylsulfanyl, heteroarylsulfanyl, amino, substituted amino, acylamino, and aminoacyl; R2is selected from the group consisting of hydrogen, deuterium, and methyl; R3 is selected from the group consisting of hydrogen, deuterium, alkyl, and substituted alkyl; R4 is selected from the group consisting of hydrogen, alkyl, and substituted alkyl; and R5 and R6 are as defined in claim 1; capable of modulating the stability and/or activity of hypoxia inducible factor (HIF).

  本发明涉及式 I 的新型化合物 其中 q 是 0 或 1； - A 是-S-，B 是＝N-；或 - A 是 =N-，B 是 -S-； -A≃C(R6)-或-B≃C(R6)-中的一个是双键，另一个是单键； R1 选自由羟基、烷氧基、取代的烷氧基、酰氧基、环烷氧基、取代的环烷氧基、芳氧基、取代的芳氧基、杂芳氧基、取代的杂芳氧基、杂环氧基、取代的杂环氧基、巯基、硫醚、取代的烷硫基、芳硫基、杂芳硫基、氨基、取代的氨基、酰氨基和氨基酰基组成的组； R2 选自氢、氘和甲基组成的组； R3 选自氢、氘、烷基和取代烷基组成的组； R4 选自由氢、烷基和取代烷基组成的组；以及 R5 和 R6 如权利要求 1 所定义； 能调节缺氧诱导因子（HIF）的稳定性和/或活性。
• Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
  申请人：Gilead Connecticut, Inc.

  公开号：US10093684B2

  公开（公告）日：2018-10-09

  Certain imidazopyrazines of Formula I and pharmaceutical compositions thereof are provided herein: Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

  本文提供了某些式 I 的咪唑吡嗪及其药物组合物： 本文提供了治疗对抑制 Syk 活性有反应的某些疾病和失调患者的方法，其中包括向这些患者施用一定量的至少一种化学实体，以有效减少疾病或失调的体征或症状。此外，还提供了确定样品中是否存在 Syk 激酶的方法。